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New compound with cativity for inhibiting glycine transport factor

A technology for inhibiting activity and glycine, applied in drug combinations, chemical instruments and methods, cyclic peptide components, etc.

Inactive Publication Date: 2004-10-13
XICHUAN INST OF ANTIBIOTIC IND NAT MEDICINE SUPERVISION BUREAU +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] No compound similar in structure to the compound of the present invention and having inhibitory activity on glycine transporters has been found so far

Method used

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  • New compound with cativity for inhibiting glycine transport factor
  • New compound with cativity for inhibiting glycine transport factor
  • New compound with cativity for inhibiting glycine transport factor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0144] Example 1 Preparation of WSS2217, WSS2218, WSS2219 and WS2220.

[0145] 1. Put the liquid culture medium containing 2.5% soluble starch, 1% glucose, 0.5% fish meal, 0.3% cottonseed meal, 0.3% NZ CASE, 0.2% yeast juice, 0.2% calcium carbonate in the Erlenmeyer flask, at 121°C , Sterilize for 20 minutes. Then, the Nonomuraea sp. TA-0426 strain was inoculated on the sterile medium, and cultured with shaking at 28° C. and 200 rpm for three days as a seed culture solution.

[0146] Then, 100ml of sterile liquid medium composed of 2% corn flour, 1.0% glycerol, 0.5% glucose, 0.5% cottonseed meal, 0.5% wort juice, 0.3% polyptone, 0.05% magnesium sulfate and 0.3% calcium carbonate Pack into a 500ml Erlenmeyer flask. 4 ml of the aforementioned seed culture solution was added thereto to prepare 100 bottles, and cultured with shaking at 28° C. and 180 rpm for 14 days.

[0147] After the cultivation, 10 L of the obtained culture solution was added to 5 L of n-butanol, stirred, ce...

Embodiment 2

[0152] The preparation of embodiment 2 WSS2221 and WSS2222

[0153] 1. Add 60ml of liquid culture medium containing 2.5% soluble starch, 1% glucose, 0.5% fish meal, 0.3% cottonseed meal, 0.3% NZ CASE, 0.2% yeast juice and 0.2% calcium carbonate into the Erlenmeyer flask, 121°C, Sterilize for 20 minutes. Then, the Nonomuraea sp. TA-0426 strain was inoculated on the sterile medium, and cultured with shaking at 28° C. and 200 rpm for three days as a seed culture solution.

[0154] Then, 100 ml of sterile liquid culture medium composed of 2% corn flour, 1.0% glycerol, 0.5% glucose, 0.5% cottonseed meal, 0.5% wort juice, 0.3% polyptone, 0.05% magnesium sulfate and 0.3% calcium carbonate Pack into a 500ml Erlenmeyer flask. 4 ml of the aforementioned seed culture solution was added thereto to prepare 150 bottles, and cultured with shaking at 28° C. and 180 rpm for 14 days.

[0155] After the cultivation, 15 L of the obtained culture solution was added to 5 L of n-butanol, stirred ...

Embodiment 3

[0158] Embodiment 3 Preparation of WSS8027

[0159] Under nitrogen flow, 1 ml of dimethylformamide was added to sodium hydroxide (100.6 mg), cooled and stirred. 1 ml of dimethylformamide in which WSS2219 (12.9 mg) was dissolved was added thereto, and methyl iodide (300 ml) was added thereto, followed by stirring at room temperature for 1 hour. After the reaction was completed, water and ethyl acetate were added under cooling in an ice bath, and the ethyl acetate layer was concentrated under reduced pressure. The concentrate was separated by high-performance liquid chromatography [mobile phase: acetonitrile-0.02% trifluoroacetic acid aqueous solution (80:20), device: Watt Company, chromatography column: ODS-AM (Φ10×150mm) manufactured by Vaem Company] , detected at 210nm, the flow rate is 2.5ml / min. The separated components were concentrated to dryness under reduced pressure to obtain 4.4 mg of WSS8027.

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Abstract

The present invention discloses conjugated of glycine with glutamic acid receptor, and can activate the receptor, the number of glycines existed in the synaptic neural gap can be regulated by glycine transferase found in the neuroglial cell, so that the inhibitor of glycine transferase can increase the glycine in the synoptic neural gap, and can be used as medicine for activating glutamic acid receptor and for curing schizophrenia. Said invention also discloses a new compound with physiological activity, said new compound has inhibiting activity for glycine transferase of glycine cell and is produced by microbial fermentation.

Description

technical field [0001] The present invention relates to novel microbially produced compounds having inhibitory activity against the glycine transporter in mammalian glial cells. technical background [0002] In recent years, studies have shown that the number of glutamate receptors in the brains of patients with schizophrenia increases significantly. The activation of glutamate receptors requires glycine present in the cerebrospinal space to bind to glutamate receptors, and the amount of glycine is regulated by the glycine transporter present in glial cells. Therefore, glycine transporter inhibitors It can increase the amount of glycine in the cerebrospinal space, so it can be used as a schizophrenia treatment drug that can activate glutamate receptors. [0003] No compound similar in structure to the compound of the present invention and capable of inhibiting glycine transporters has been found so far. Contents of the invention [0004] The object of the present inventi...

Claims

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Application Information

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IPC IPC(8): A61K38/12A61P25/00C07K5/12
Inventor 褚以文李俊英户田喜久照井佑一福永拓哉
Owner XICHUAN INST OF ANTIBIOTIC IND NAT MEDICINE SUPERVISION BUREAU
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